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SELF-ASSEMBLY FOR ACTIVATING IMMUNITY

Foreign code F200010048
File No. 6202
Posted date May 14, 2020
Country WIPO
International application number 2019JP033920
International publication number WO 2020045570
Date of international filing Aug 29, 2019
Date of international publication Mar 5, 2020
Priority data
  • P2018-161582 (Aug 30, 2018) JP
Title SELF-ASSEMBLY FOR ACTIVATING IMMUNITY
Abstract Provided are: a novel compound that forms a self-assembly; the self-assembly; production methods for the compound and the self-assembly; and pharmaceutical use of the compound and the self-assembly. The compound is represented by formula (I) [in the formula, Rx represents H or a group represented by formula (II), Ry represents H or a group represented by formula (III), R1, R2, R3, and R4 each independently represent H, C1-6 alkyl, or C1-6 haloalkyl, a wavy line represents a binding site, and n represents an integer of 1-12]. The self-assembly is formed by the composition. The production methods are for the compound and the self-assembly, and the pharmaceutical use are for the compound and the self-assembly.
Outline of related art and contending technology BACKGROUND ART
Biological in vivo in the formation of a hierarchical structure, such as self-assembly of molecules spontaneously self-assembled is an important role. For example, DNA, lipid membrane and cytoskeletal fibers and the like are an example of the natural self-assembly. In general, a single compound having a single function of the molecules on the other hand, the self-assembly in accordance with the ambient environment or complex physical and chemical properties of the (non-patent document 1) function. Therefore, the synthesis of the new self-assembly, a biological system to modulate the activity or biological function of a new drug development has been attracting attention as one of techniques.
Immunopotentiators action of the biological activity, age 1920 using the aluminum compound since adjuvant have been developed, a variety of immune activation agent such as diphtheria or influenza infections disease vaccine used. Is immunopotentiators of these, such as Toll-like receptor (TLR) by acting on the pattern recognition receptors of the immune cells are activated and, for example non-methylated CG (CpG-ODN) or synthetic oligonucleotides comprising sequences and the like have been known (Non-Patent Document 2). In this way, natural self-assembly of self-assembly in a manner similar to the structure have been reported that some, most of the peptide and a constituent unit of the self-assembly. Non-peptide synthesis may be an example of a self-assembly of chemical molecules have been known some embodiments, the biological activity of their toxicity and primarily relates to cell death (Non-Patent Document 3-10). Therefore, the biological activity of the new and useful additional synthetic chemical molecule self-assembly has been desired.
Scope of claims (In Japanese)[請求項1]
 式(I):
[化1]
(省略)
[式中、R xは、H又は式(II):
[化2]
(省略)
で示される基であり、
 R yは、H又は式(III):
[化3]
(省略)
で示される基であり、
 R 1、R 2、R 3及びR 4は、それぞれ独立して、H、C 1-6アルキル又はC 1-6ハロアルキルであり、
 波線は結合部位を示し、
 nは1~12の整数である]
で示される化合物が非共有結合により連結してなる、自己集合体。

[請求項2]
 R xがR yと同一である、請求項1に記載の自己集合体。

[請求項3]
 R xが式(II’):
[化4]
(省略)
で示される基であり、
 R yが式(III’):
[化5]
(省略)
で示される基である、請求項1又は2に記載の自己集合体。

[請求項4]
 R 3及びR 4がそれぞれ独立してC 1-3アルキルである、請求項1~3のいずれかに記載の自己集合体。

[請求項5]
 R x及びR yがともにHである、請求項1又は2に記載の自己集合体。

[請求項6]
 nが5~10の整数である、請求項1~5のいずれかに記載の自己集合体。

[請求項7]
 流体力学的サイズ40nm~12,000nmを有する凝集体を形成する、請求項1~6のいずれかに記載の自己集合体。

[請求項8]
 請求項1~7のいずれかに記載の自己集合体を含む、免疫賦活剤。

[請求項9]
 アジュバントである、請求項8に記載の免疫賦活剤。

[請求項10]
 請求項9に記載の免疫賦活剤及び抗原を含む、ワクチン組成物。

[請求項11]
 がん、感染症、アレルギー疾患、自己免疫疾患、高血圧症及びアルツハイマー病からなる群から選択される疾患の治療及び/又は予防のための、請求項10に記載のワクチン組成物。

[請求項12]
 式(I):
[化6]
(省略)
[式中、R xは、H又は式(II):
[化7]
(省略)
で示される基であり、
 R yは、H又は式(III):
[化8]
(省略)
で示される基であり、
 R 1、R 2、R 3及びR 4は、それぞれ独立して、H、C 1-6アルキル又はC 1-6ハロアルキルであり、
 波線は結合部位を示し、
 nは1~12の整数である]
で示される化合物。
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • KYOTO UNIVERSITY
  • OSAKA UNIVERSITY
  • Inventor
  • UESUGI, Motonari
  • VU, Hue T.
  • YOSHIDA, Hiroki
  • NODA, Naotaka
  • JIN, Shuyu
  • YAMASAKI, Sho
  • SHIMANE, Toru
  • ISHII, Ken
  • HIOKI, Kou
IPC(International Patent Classification)
Specified countries National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DJ DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JO JP KE KG KH KN KP KR KW KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN ST TD TG
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